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• Organic nitrates
•  receptor blockers
• Calcium channel blockers
Coronary vessels: blood supply for the heart
1. OVERVIEW
Coronary atherosclerosis:
cause of cardiac ischemia
 Generally described as
retrosternal heavy or
gripping sensation with
radiation to left arm or neck,
provoked by exertion and
eased with rest or nitrates
 AP-the chief symptom of ischemic heart
disease, is due to imbalance bet O2 supply &
O2 demand of the myocardium.
 Symptoms :sudden, severe, substernal
discomfort or pain which may radiate to the
left shoulder & along the flexor surface of the
left arm.
 O2 consumption depends on preload (venous
return & streching of the heart ),& afterload
(PVR) & HR.
 1 Stable angina :(classical angina, angina of
effort, exertional angina)-pain is induced by
exercise or emotion, both increases O2 demand.
 2 Unstable angina ( angina at rest) : common
due to rupture of an atheromatous plaque &
platelet deposition in the coronary artery, leading
to progressive thrombosis. (here patients of
stable angina develops angina at rest )
 3 prinzmetal’angina : (variant angina) – angina
that develops at rest & is due to spasm of the
coronary arteries.
 O2supplydecreases
 Coronary
atherosclerosis
 Coronary
vasospasm
 Coronary
thrombosis
 O2 demand
increases
 Increase HR
 Ventricular
hypertrophy
 Increased
ventricular
contractility
 Increased
ventricular wall
tension.
 Increasing O2 supply
 Remove athero.
Plaque
 Remove vasospasm
by drugs –
CCBS,NITRATES
 Break the thrombi-
strepto. Uro.
 Prevent thrombi -
aspirin
 Decreasing O2
demand
 By reducing
workload as preload
–nitrates
 Afterload –CCBS
 Decreases HR &
contractility -BBS
1. Nitrates: Nitroglycerine, ISDN, ISMN.
2. CCBS : Verapamil, Diltiazam, Nifedipine,
Amlodipine.
3. BBS: Propranolol, Atenolol.
4. Potassium channel openers: Nicorandil
5. Miscellaneous: low dose aspirin,
dipyridamole, trimetazidine.
 Nitrates are prodrugs & they release nitric
oxide (NO).
 Nitrates are mainly venodilators, also cause
arteriolar dilatation & as a result reduce both
Preload & Afterload.
NITRATES
Denitrated in the smooth muscle cell
Releases nitric oxide
Stimulates guanylyl cyclase
Increases cGMP –This cGMP catalyses the
phosphorylation of protein kinases causing
relaxation of the smooth muscles.
 Nitroglycerine (NTG): quickly relieves pain by
decre. O2 requirement & incre. O2 supply to
the myocardium.
 NTGs are predominantly venodilators.
 Venodilatation reduces venous return to the
heart, thereby reduces preload.
 Arteriolar dilatation reduces PVR = decre. In
Afterload.( so decre. O2 requirement).
 In variant angina , Nitrates relieve vasospasm
due to coronary vasodilation.
 Nitrates cause dilatation of blood vessels in
the skin = flushing
 Dilatation of meningeal vessels =headache.
 Bronchial smooth muscles are also relaxed.
 Nitrates are well absorbed orally but undergo
extensive 1st-pass metabolism.
 Sublingual route =rapid onset (2 to 5 min)
but short duration of action.
 Absorption through skin is slow, so used for
prolonged effect.
 Metabolites are excreted in urine as
glucuronide derivatives.
 Headache ,flushing, sweating, palpitation,
weakness, postural hypotension & rashes can
occur.
 Tolerance (also cross tolerance)
 By proper dosage schedule ,tolerance can be
avoided.( 8 hr drug free interval )
 Also tolerance minimised by twice/thrice
daily dosage schedule.
1. Angina: sublingual NTG are DOC.
◦ Repeated 3 tab in 15 min.
◦ LA nitrates are used orally for prophylaxis of
angina.
◦ NTG ointment may be applied over the chest.
2. Cardiac failure: as a vasodilator.
3. MI: IV NTG used for decreasing cardiac
work.
4. Biliary colic: sublingual NTG are used to
relieve biliary spasm .
 5 cyanide poisoning : cyanide rapidly binds to
cytochrome oxidase = inhibition of cellular
respiration & blocks the utilization of O2.
 TREATMENT:
HB METHB CYANOMETHB
iv sod thiosul.
SODIUMTHIOCYANATE
CYANIDE (rapidly ex.in uri)
CYTOCHROME OXIDASE
nitrite
 CCBS relax the arterioles leading to decrease
in PVR & reduction in Afterload.
 Also depress myo. Contractility thereby
reduces HR & FOC.
 This results in reduced cardiac workload & O2
consumption.
 CCBS also dilate the coronaries thereby
increases coronary blood flow.
 CCBS :Used for prophylaxis of exertional
angina.
 They can be combined ( except verapamil)
with BB.
 CCBS are also used in vasospastic angina
since they dilate the coronaries & relieve
vasospasm. ( preffered over nitrares.)
 BBS reduces the severity of attacks of
exertional angina & are useful in the
prevention of angina.
 Exercise,emotion etc. increases sympa.
Activity = incre. In HR, FOC & BP, therefor
increase in O2 consumption.
 BBS prevent angina by blocking all these
actions.
 Used for longterm prophylaxis of classical
angina& may be combined with nitrates.
 BBS should always be tappered after
prolonged use.
 Not useful in variant angina.
 Nicorandil-an arterial & venous dilator.
 Opening of the ATP sensitive K+ channels
=efflux of K+ =hyperpolarisation & so
relaxation of the vascular smooth muscles.
 Also acts through NO like Nitrates.
 expensive
 Has LA & does not cause tolerance.
 S/es =Headache,flushing,palpitation,dizziness &
hypotension.
 Pinacidil is = to Nicorandil & is useful in AP&
HTN.
 Dipyridamole :coronary vasodilator but it
diverts blood from ischaemic zone &so not
beneficial. (used in platelet aggre. Prevention)
 Aspirin ;long term admini. Of a low dose for
preventing MI.
 Trimetazidine :a CCB claimed to have a
protective effect on the ischaemic
myocardium & to maintain left ven. Function.
 Used in exertional angina - 20 mg TDS.

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ANGINA PECTORIS-bpt.pptx

  • 1. • Organic nitrates •  receptor blockers • Calcium channel blockers
  • 2. Coronary vessels: blood supply for the heart 1. OVERVIEW
  • 4.  Generally described as retrosternal heavy or gripping sensation with radiation to left arm or neck, provoked by exertion and eased with rest or nitrates
  • 5.  AP-the chief symptom of ischemic heart disease, is due to imbalance bet O2 supply & O2 demand of the myocardium.  Symptoms :sudden, severe, substernal discomfort or pain which may radiate to the left shoulder & along the flexor surface of the left arm.  O2 consumption depends on preload (venous return & streching of the heart ),& afterload (PVR) & HR.
  • 6.  1 Stable angina :(classical angina, angina of effort, exertional angina)-pain is induced by exercise or emotion, both increases O2 demand.  2 Unstable angina ( angina at rest) : common due to rupture of an atheromatous plaque & platelet deposition in the coronary artery, leading to progressive thrombosis. (here patients of stable angina develops angina at rest )  3 prinzmetal’angina : (variant angina) – angina that develops at rest & is due to spasm of the coronary arteries.
  • 7.  O2supplydecreases  Coronary atherosclerosis  Coronary vasospasm  Coronary thrombosis  O2 demand increases  Increase HR  Ventricular hypertrophy  Increased ventricular contractility  Increased ventricular wall tension.
  • 8.  Increasing O2 supply  Remove athero. Plaque  Remove vasospasm by drugs – CCBS,NITRATES  Break the thrombi- strepto. Uro.  Prevent thrombi - aspirin  Decreasing O2 demand  By reducing workload as preload –nitrates  Afterload –CCBS  Decreases HR & contractility -BBS
  • 9. 1. Nitrates: Nitroglycerine, ISDN, ISMN. 2. CCBS : Verapamil, Diltiazam, Nifedipine, Amlodipine. 3. BBS: Propranolol, Atenolol. 4. Potassium channel openers: Nicorandil 5. Miscellaneous: low dose aspirin, dipyridamole, trimetazidine.
  • 10.  Nitrates are prodrugs & they release nitric oxide (NO).  Nitrates are mainly venodilators, also cause arteriolar dilatation & as a result reduce both Preload & Afterload.
  • 11.
  • 12. NITRATES Denitrated in the smooth muscle cell Releases nitric oxide Stimulates guanylyl cyclase Increases cGMP –This cGMP catalyses the phosphorylation of protein kinases causing relaxation of the smooth muscles.
  • 13.
  • 14.  Nitroglycerine (NTG): quickly relieves pain by decre. O2 requirement & incre. O2 supply to the myocardium.  NTGs are predominantly venodilators.  Venodilatation reduces venous return to the heart, thereby reduces preload.  Arteriolar dilatation reduces PVR = decre. In Afterload.( so decre. O2 requirement).  In variant angina , Nitrates relieve vasospasm due to coronary vasodilation.
  • 15.  Nitrates cause dilatation of blood vessels in the skin = flushing  Dilatation of meningeal vessels =headache.  Bronchial smooth muscles are also relaxed.
  • 16.  Nitrates are well absorbed orally but undergo extensive 1st-pass metabolism.  Sublingual route =rapid onset (2 to 5 min) but short duration of action.  Absorption through skin is slow, so used for prolonged effect.  Metabolites are excreted in urine as glucuronide derivatives.
  • 17.  Headache ,flushing, sweating, palpitation, weakness, postural hypotension & rashes can occur.  Tolerance (also cross tolerance)  By proper dosage schedule ,tolerance can be avoided.( 8 hr drug free interval )  Also tolerance minimised by twice/thrice daily dosage schedule.
  • 18. 1. Angina: sublingual NTG are DOC. ◦ Repeated 3 tab in 15 min. ◦ LA nitrates are used orally for prophylaxis of angina. ◦ NTG ointment may be applied over the chest. 2. Cardiac failure: as a vasodilator. 3. MI: IV NTG used for decreasing cardiac work. 4. Biliary colic: sublingual NTG are used to relieve biliary spasm .
  • 19.  5 cyanide poisoning : cyanide rapidly binds to cytochrome oxidase = inhibition of cellular respiration & blocks the utilization of O2.  TREATMENT: HB METHB CYANOMETHB iv sod thiosul. SODIUMTHIOCYANATE CYANIDE (rapidly ex.in uri) CYTOCHROME OXIDASE nitrite
  • 20.  CCBS relax the arterioles leading to decrease in PVR & reduction in Afterload.  Also depress myo. Contractility thereby reduces HR & FOC.  This results in reduced cardiac workload & O2 consumption.  CCBS also dilate the coronaries thereby increases coronary blood flow.  CCBS :Used for prophylaxis of exertional angina.
  • 21.  They can be combined ( except verapamil) with BB.  CCBS are also used in vasospastic angina since they dilate the coronaries & relieve vasospasm. ( preffered over nitrares.)
  • 22.  BBS reduces the severity of attacks of exertional angina & are useful in the prevention of angina.  Exercise,emotion etc. increases sympa. Activity = incre. In HR, FOC & BP, therefor increase in O2 consumption.  BBS prevent angina by blocking all these actions.  Used for longterm prophylaxis of classical angina& may be combined with nitrates.
  • 23.  BBS should always be tappered after prolonged use.  Not useful in variant angina.
  • 24.  Nicorandil-an arterial & venous dilator.  Opening of the ATP sensitive K+ channels =efflux of K+ =hyperpolarisation & so relaxation of the vascular smooth muscles.  Also acts through NO like Nitrates.  expensive  Has LA & does not cause tolerance.  S/es =Headache,flushing,palpitation,dizziness & hypotension.  Pinacidil is = to Nicorandil & is useful in AP& HTN.
  • 25.  Dipyridamole :coronary vasodilator but it diverts blood from ischaemic zone &so not beneficial. (used in platelet aggre. Prevention)  Aspirin ;long term admini. Of a low dose for preventing MI.  Trimetazidine :a CCB claimed to have a protective effect on the ischaemic myocardium & to maintain left ven. Function.  Used in exertional angina - 20 mg TDS.